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Assay Detail

CHEMBL1937263

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Inhibition of LPS-induced TNFalpha production in human PBMC pre-incubated for 30 mins prior to LPS-induction measured after 4 hrs by ELISA
ChEMBL ↗
36
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type PBMC
Confidence 1 — Organism
Curated By Autocuration

Target

PBMC (CHEMBL613107) ↗
Type CELL-LINE
Organism Homo sapiens

Publication

Novel ATP competitive MK2 inhibitors with potent biochemical and cell-based activity throughout the series.
Oubrie A, Kaptein A, de Zwart E, Hoogenboom N, Goorden R, van de Kar B, van Hoek M, de Kimpe V, van der Heijden R, Borsboom J, Kazemier B, de Roos J, Scheffers M, Lommerse J, Schultz-Fademrecht C, Barf T.
Bioorg Med Chem Lett (2012) 22 : 613 -618
PubMed 22119462 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 36 6.65 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1933182 — — 1 7.52
CHEMBL1933172 — — 1 7.52
CHEMBL1933178 — — 3 7.40
CHEMBL1933174 — — 1 7.30
CHEMBL1933179 — — 3 7.16
CHEMBL1933170 — — 1 7.16
CHEMBL1933181 — — 3 7.16
CHEMBL1933185 — — 1 6.89
CHEMBL1933187 — — 1 6.85
CHEMBL1933186 — — 1 6.85
CHEMBL1933171 — — 1 6.82
CHEMBL1933188 — — 1 6.82
CHEMBL1933173 — — 1 6.80
CHEMBL1933191 — — 1 6.77
CHEMBL1933190 — — 1 6.70
CHEMBL1933183 — — 1 6.70
CHEMBL1933164 — — 1 6.64
CHEMBL1738702 — — 1 6.58
CHEMBL1933176 — — 1 6.58
CHEMBL1933180 — — 1 6.41
CHEMBL1933184 — — 1 6.32
CHEMBL1933166 — — 1 6.19
CHEMBL1933192 — — 1 6.19
CHEMBL1933162 — — 1 6.05
CHEMBL1933168 — — 1 5.85
CHEMBL1933175 — — 1 5.80
CHEMBL1933177 — — 1 5.58
CHEMBL1933189 — — 1 -
CHEMBL1933169 — — 1 -
CHEMBL1933193 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1933182 — EC50 = 30.0 nM 7.52
CHEMBL1933172 — EC50 = 30.0 nM 7.52
CHEMBL1933178 — EC50 = 40.0 nM 7.40
CHEMBL1933174 — EC50 = 50.0 nM 7.30
CHEMBL1933170 — EC50 = 70.0 nM 7.16
CHEMBL1933179 — EC50 = 70.0 nM 7.16
CHEMBL1933181 — EC50 = 70.0 nM 7.16
CHEMBL1933181 — EC50 = 70.0 nM 7.16
CHEMBL1933185 — EC50 = 130.0 nM 6.89
CHEMBL1933186 — EC50 = 140.0 nM 6.85
CHEMBL1933187 — EC50 = 140.0 nM 6.85
CHEMBL1933188 — EC50 = 150.0 nM 6.82
CHEMBL1933171 — EC50 = 150.0 nM 6.82
CHEMBL1933173 — EC50 = 160.0 nM 6.80
CHEMBL1933179 — EC50 = 170.0 nM 6.77
CHEMBL1933191 — EC50 = 170.0 nM 6.77
CHEMBL1933183 — EC50 = 200.0 nM 6.70
CHEMBL1933190 — EC50 = 200.0 nM 6.70
CHEMBL1933164 — EC50 = 230.0 nM 6.64
CHEMBL1933176 — EC50 = 260.0 nM 6.58
CHEMBL1738702 — EC50 = 260.0 nM 6.58
CHEMBL1933180 — EC50 = 390.0 nM 6.41
CHEMBL1933184 — EC50 = 480.0 nM 6.32
CHEMBL1933166 — EC50 = 650.0 nM 6.19
CHEMBL1933192 — EC50 = 650.0 nM 6.19
CHEMBL1933162 — EC50 = 890.0 nM 6.05
CHEMBL1933178 — EC50 = 1200.0 nM 5.92
CHEMBL1933168 — EC50 = 1400.0 nM 5.85
CHEMBL1933175 — EC50 = 1600.0 nM 5.80
CHEMBL1933181 — EC50 = 1600.0 nM 5.80
CHEMBL1933177 — EC50 = 2600.0 nM 5.58
CHEMBL1933178 — EC50 - — -
CHEMBL1933179 — EC50 - — -
CHEMBL1933189 — EC50 - — -
CHEMBL1933169 — EC50 - — -
CHEMBL1933193 — EC50 - — -